• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    …<CHEM>… and salts thereof wherein n is an integer from 1 to 5, X is a chalcogen and R is hydrogen or lower alkyl and methods of preparation. The derivatives are useful for treating or preventing diabetic complications.
    公开号:SU1468897A1
    申请号:SU853976227
    申请日:1985-11-11
    公开日:1989-03-30
    发明作者:Беллини Франческо；Сестан Казимир
    申请人:Айерст,Маккенна Энд Хэррисон Инк. (Фирма)；
    IPC主号:
    专利说明:

    Note L, N and D values illustrate the percentage reduction.
    the degree of accumulation of dulcite in the tissues of the lens of the eyes, sciatic nerves and diaphragm, respectively.
    权利要求:
    Claims (2)
    [1]
    ^ Claims
    N- [b-Methoxy-5- (perfluoroalkyl) - '
    -1-naphthoyl] -N-methylglycine or its : thionaphthoyl analogues of the formula!
    or 2
    -soon where n «1 or n = 2, X = -0,
    45 as an inhibitor of aldose reduction of 1 pelvis.
    Test compound η X Degree of% 10 * 7 M Vitro inhibiin Reduced accumulated dulcite in vivo,%ΞΞΕΊΞ Name mg / kg / day
    N- ^ 5- (Pentafluoroethyl) -6-methoxy1-naphthalenyl] thioxomethyl ^ -N-methylglycine
    Ν- [[5- (Heptafluoropropyl) -6-label- ’si-1-naphthalenyl} thioxomethox} -N-methylglycine
    Ν- [£ 5- (Heptafluoropropyl) -6-methoxy-1-naphthalenyl ^ carbonyl} -N-methylglycine
    N [(5- (Trifluoromethyl) -5-methoxy-1-naphthalenyl] thioxomethyl ^ —N-methylglycine
    Tolrestat (known compound)
    1UNIT so -3.5 Sin nerveg / kg 71 24.551 2 S 75 5,025
    [2]
    2 0 63
    10.0
    50,0
    0 79 4.0
    11.0
    EDV Nerve 6.4 mg / kg
    ED50 - in crunch. - 178 26 mg / kg
    29 93 93
    16 20 52 76
    NS 83 84
    19 45 38 18 52 59
    0 35 80 14 86 89 fifteen - -
    Note. Values L, N and D illustrate the percentage reduction in the degree of accumulation of dulcite in the tissues of the lenses of the eyes, sciatic nerves and diaphragm, respectively.
    类似技术:
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    同族专利:
    公开号 | 公开日
    EP0182499B1|1989-04-12|
    UA7051A1|1995-03-31|
    DK166147B|1993-03-15|
    DK529585D0|1985-11-15|
    JPH0611739B2|1994-02-16|
    HUT42059A|1987-06-29|
    KR860004010A|1986-06-16|
    ES8801619A1|1988-02-16|
    IE58620B1|1993-10-20|
    AT42091T|1989-04-15|
    EP0182499A1|1986-05-28|
    DE3569367D1|1989-05-18|
    IE852598L|1986-05-16|
    KR900006128B1|1990-08-24|
    JPS61122256A|1986-06-10|
    DK529585A|1986-05-17|
    GR852726B|1986-03-13|
    ES548914A0|1988-02-16|
    HU194159B|1988-01-28|
    CA1253520A|1989-05-02|
    AU583311B2|1989-04-27|
    AU4898185A|1986-05-22|
    US4604406A|1986-08-05|
    DK166147C|1993-08-09|
    PH21450A|1987-10-28|
    ZA858186B|1987-06-24|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    US4254108A|1979-11-08|1981-03-03|Ayerst, Mckenna & Harrison Inc.|Thioxo-1H-benz[de]isoquinoline-2-acetic acid derivatives and antidiabetic use thereof|
    US4254109A|1979-11-08|1981-03-03|Ayerst, Mckenna & Harrison Inc.|1H-Benz[de]isoquinoline-2-acetic acid derivatives|
    AU544067B2|1981-03-02|1985-05-16|Wyeth-Ayerst Canada Inc.|Thioamides and amides. treatment of diabetes|
    CA1176269A|1981-03-02|1984-10-16|Kazimir Sestanj|N-naphthoylglycine derivatives|
    CA1147739A|1981-03-02|1983-06-07|Kazimir Sestanj|N-aminoacid derivatives|
    CA1182472A|1981-03-02|1985-02-12|Kazimir Sestanj|N-[thioxomethyl]glycinederivatives|
    US4369188A|1981-07-17|1983-01-18|Ayerst, Mckenna & Harrison Inc.|2-Thioxobenz[cd]indole-1-acetic acid derivatives|
    CA1191156A|1981-10-15|1985-07-30|Francesco Bellini|N--5--1-naphthalenyl)-thioxomethyl)-n-glycines|US4822904A|1985-12-12|1989-04-18|Ethyl Corporation|Perfluoroalkylation process|
    US4699993A|1985-12-12|1987-10-13|Ethyl Corporation|Perfluoroalkylnaphthalene compounds|
    US4734435A|1986-04-07|1988-03-29|American Home Products Corp.|N-[[6-methoxy-5--1-naphthalenyl]-thioxomethyl]-N-methylglycine S-oxide and the amide thereof|
    JPS6399057A|1986-06-27|1988-04-30|Nippon Shinyaku Co Ltd|Glycine derivative|
    US4731380A|1986-08-26|1988-03-15|American Home Products Corporation |Tolerstat as an agent for diabetic periodontitis|
    AU598366B2|1987-03-20|1990-06-21|Alcon Laboratories, Inc.|Use of aldose reductase inhibitors to enhance insulin sensitivity in diabetes|
    JP2548258Y2|1990-12-21|1997-09-17|ペガサスミシン製造株式会社|Automatic lip stitching device|
    US5388146A|1991-11-12|1995-02-07|Microlog Corporation|Automated telephone system using multiple languages|
    US5337844A|1992-07-16|1994-08-16|Baker Hughes, Incorporated|Drill bit having diamond film cutting elements|
    US20150057452A1|2012-04-04|2015-02-26|Catylix, Inc.|Selective androgen receptor modulators|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    US06/672,015|US4604406A|1984-11-16|1984-11-16|N-[6-methoxy-5--1-naphtholyl]-N-methylglycines and their thionaphthoyl analogs|LTRP1132A| LT2592B|1984-11-16|1993-09-27|N--1-NAFTOYL) -N-METHYLLYCIN OR TIONAFTOILIC ANALYZES AS ALDOZOREDUCTAESE INHIBITORS|
    LV931190A| LV5614A3|1984-11-16|1993-11-11|N-U6-Methoxy-5--1-naphthalenyl-N-methylglycine and thionaphthylanalogs, aldose reductase inhibitors|
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